KRAS: From undruggable to a druggable Cancer Target

D Uprety, AA Adjei - Cancer treatment reviews, 2020 - Elsevier
RAS is the most frequently mutated oncogene in human cancers, with mutations in about
30% of all cancers. RAS exists in three different isoforms (K-RAS, H-RAS and N-RAS) with …

The current state of the art and future trends in RAS-targeted cancer therapies

SR Punekar, V Velcheti, BG Neel… - Nature reviews Clinical …, 2022 - nature.com
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …

Progress in targeting RAS with small molecule drugs

F McCormick - Biochemical Journal, 2019 - portlandpress.com
RAS proteins have traditionally been deemed undruggable, as they do not possess an
active site to which small molecules could bind but small molecules that target one form of …

[HTML][HTML] Therapeutic targeting of RAS: New hope for drugging the “undruggable”

I Khan, JM Rhett, JP O'Bryan - … et Biophysica Acta (BBA)-Molecular Cell …, 2020 - Elsevier
RAS is the most frequently mutated oncogene in cancer and a critical driver of oncogenesis.
Therapeutic targeting of RAS has been a goal of cancer research for more than 30 years …

Targeting KRAS in Cancer: Promising Therapeutic Strategies

LM Mustachio, A Chelariu-Raicu, L Szekvolgyi… - Cancers, 2021 - mdpi.com
Simple Summary Since the Kirsten rat sarcoma viral oncogene homolog (KRAS) is mutated
in about 25% of all human cancers and is at the center of pathways involved in …

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

JML Ostrem, KM Shokat - Nature reviews Drug discovery, 2016 - nature.com
KRAS is the most frequently mutated oncogene in human cancer. In addition to holding this
distinction, unsuccessful attempts to target this protein have led to the characterization of …

Classification of KRAS-Activating Mutations and the Implications for Therapeutic Intervention

C Johnson, DL Burkhart, KM Haigis - Cancer discovery, 2022 - AACR
Members of the family of RAS proto-oncogenes, discovered just over 40 years ago, were
among the first cancer-initiating genes to be discovered. Of the three RAS family members …

[HTML][HTML] Targeting the untargetable KRAS in cancer therapy

P Liu, Y Wang, X Li - Acta Pharmaceutica Sinica B, 2019 - Elsevier
RAS is one of the most well-known proto-oncogenes. Its gain-of-function mutations occur in
approximately 30% of all human cancers. As the most frequently mutated RAS isoform …

Improving prospects for targeting RAS

H Singh, DL Longo, BA Chabner - Journal of clinical oncology, 2015 - ascopubs.org
RAS mutations are among the most common oncogenic drivers in human cancers, affecting
nearly a third of all solid tumors and around a fifth of common myeloid malignancies, but …

Targeting KRAS in solid tumors: current challenges and future opportunities of novel KRAS inhibitors

A Indini, E Rijavec, M Ghidini, A Cortellini, F Grossi - Pharmaceutics, 2021 - mdpi.com
Activating mutations in RAS family proteins are found in~ 25% of all human cancers.
Different solid tumors are correlated with mutations in certain isoforms of RAS, with Kirsten …